Assay Detail

CHEMBL1028105

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Binding

Inhibition of human PKCeta

ChEMBL ↗

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Target

Protein kinase C eta type (CHEMBL3616) ↗

Open DB target context

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Protein kinase C eta type (CHEMBL3616) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Protein kinase C eta type

CHEMBL3616

Anchored from Assay target.

Protein identity Protein kinase C eta type

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Protein kinase C eta type (CHEMBL3616) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase.

Heerding DA, Rhodes N, Leber JD, Clark TJ, Keenan RM, Lafrance LV, Li M, Safonov IG, Takata DT, Venslavsky JW, Yamashita DS, Choudhry AE, Copeland RA, Lai Z, Schaber MD, Tummino PJ, Strum SL, Wood ER, Duckett DR, Eberwein D, Knick VB, Lansing TJ, McConnell RT, Zhang S, Minthorn EA, Concha NO, Warren GL, Kumar R.
J Med Chem (2008) 51 : 5663 -5679
PubMed 18800763 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	8.70	8.70

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL494089	GSK-690693	1.0	1	8.70

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL494089	GSK-690693	IC50	=	2.0	nM	8.70